Insilico Medicine (“Insilico”), a clinical stage artificial intelligence (AI)-driven drug R&D company, today announces positive topline results of safety, tolerability, and pharmacokinetics (PK) from the Phase I clinical trial of INS018_055, a potential first-in-class drug discovered by Insilico's end-to-end AI platform for idiopathic pulmonary fibrosis (IPF).
"Topline data from our Phase 1 study of INS018_055 demonstrate the ability of our Pharma.AI platform to discover novel targets and design novel molecules with a high level of translatability to human biology,” said Alex Zhavoronkov, PhD, Founder and CEO of Insilico Medicine. “This lead program is paving the way for a new era of drug discovery and development that utilizes next generation AI to identify novel targets and generate novel drugs to treat diseases requiring regular peroral drug administration for the entire lifetime with very high safety requirements.”
Idiopathic pulmonary fibrosis (IPF) is a type of chronic scarring lung disease characterized by a progressive and irreversible decline in lung function affecting around 5 million people globally. IPF carries a poor prognosis with a median survival of 3 to 4 years and represents a significant unmet medical need. INS018_055 is the first anti-fibrotic small molecule inhibitor generated by Insilico's Pharma.AI drug discovery platform with a novel target discovered and novel structure designed by AI.
The INS018_055 Phase 1 study was a randomized, double-blind, placebo-controlled Phase 1 study featured a single ascending dose (SAD) and multiple ascending dose (MAD) to evaluate the safety, tolerability, PK, food effects, and drug-drug interaction (DDI) potential of INS018_055 in 78 healthy volunteers in New Zealand (NZ). Enrollment in Insilico Medicine’s Phase 1 clinical trial was initiated in Feb. 2022 and the last subject follow-up visit was completed in Nov. 2022. The safety and PK data collection has been completed for both SAD and MAD cohorts.
The observed human PK of INS018_055 in healthy volunteers was in line with the Company’s preclinical modeling with no significant accumulation after 7 days and exhibited a favorable PK profile. INS018_055 was generally safe and well tolerated by healthy volunteers in the study. There were no deaths or SAEs reported during the study. One subject receiving INS018_055 in the MAD 30 mg once daily cohort discontinued the study treatment due to a moderate TEAE of influenza-like illness, which was considered unrelated to the study treatment. All treatment-related AEs were of mild severity and resolved by the end of the study.
Based on these results, Insilico expects to initiate a Phase 2a study of INS018_055 in IPF patients in early 2023. The company expects to share additional data from this Phase 1 study in future updates.
“There remains a high unmet medical need for idiopathic pulmonary fibrosis, and INS018_055 targets major activated signaling cascades that significantly contribute to the pathogenesis of lung fibrosis with both anti-fibrotic and anti-inflammatory activity,” said Sujata Rao, MD, SVP, Head of Global Clinical Development at Insilico Medicine. “Results from this study are promising for safety and tolerability of INS018_055 and will be incorporated into a regulatory submission to the FDA. Pending approval by the Agency, we expect initiation of the Phase 2a study in early 2023.”
“INS018_055 is the first AI-designed novel molecule for an AI-discovered novel target entered into a clinical trial,” said Feng Ren, PhD, Chief Scientific Officer and co-CEO of Insilico Medicine.“The topline data demonstrate good PK and tolerability of the drug in healthy volunteers in both SAD and MAD, which is quite encouraging. The positive Phase I data enable the further evaluation of the drug efficacy in IPF patients in the Phase 2 trial. In addition, the continued progression of INS018_055 demonstrates again the power of our AI platform in drug discovery and development.”
For more information about Insilico's clinical trial please visit ClinicalTrials.gov (Identifier NCT05154240).
About Insilico Medicine
Insilico Medicine, a clinical stage end-to-end artificial intelligence (AI)-driven drug discovery company, is connecting biology, chemistry, and clinical trials analysis using next-generation AI systems. The company has developed AI platforms that utilize deep generative models, reinforcement learning, transformers, and other modern machine learning techniques for novel target discovery and the generation of novel molecular structures with desired properties. Insilico Medicine is developing breakthrough solutions to discover and develop innovative drugs for cancer, fibrosis, immunity, central nervous system diseases, infectious diseases, autoimmune diseases, and aging-related diseases.